scholarly journals TO STUDY THE IN VITRO INHIBITION OF BLOOD PLATELET AGGREGATION BY ISOLATED COMPOUNDS FROM CLAUSENA DENTATA (WILLD.) ROEM.

2019 ◽  
pp. 128-133
Author(s):  
ANNAMALAI MADURAM ◽  
RAJU KAMARAJ
Keyword(s):  
Platelet Aggregation ◽  
Tamil Nadu ◽  
Adenosine Diphosphate ◽  
Blood Platelet ◽  
Stem Bark ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity ◽  
Treatment Of Wounds ◽  
Trees And Shrubs

Objectives: The objectives of the study were to study the antiplatelet aggregation activity of compounds isolated from extracts of Clausena dentata. Clausena (Rutaceae) is a genus of about 23 species of unarmed trees and shrubs. The stem bark of C. dentata is used in veterinary medicine for the treatment of wounds and sprains. Even though C. dentata has a lot of potential medical uses, the study of pharmacological properties is very scarce. Methods: The plant C. dentata was collected from Kadagaman, near Tiruvannamalai, Tamil Nadu, India, and authenticated by Centre for Advanced Study in Botany, University of Madras, Chennai. The dry powder of stem bark was extracted with hexane, chloroform, and methanol. The extracts were subjected to qualitative phytochemical screening and column chromatography. Four compounds were isolated. All the isolated compounds were subjected to adenosine diphosphate (ADP)-induced platelet aggregation and compared with aspirin. Results: The isolated compounds from C. dentata and standard aspirin showed significant antiplatelet activity against ADP-induced platelet aggregation. Conclusion: The compounds, 3-(1,1-dimethylallyl)xanthyletin, dentatin, nordentatin, and carbazole showed significant antiplatelet aggregation activity. Among the compounds, nordentatin showed more activity of antiplatelet aggregation.

Triterpenoids with Antiplatelet Aggregation Activity from the Roots of Ilex pubescens

Planta Medica ◽  
2016 ◽  
Vol 83 (09) ◽  
pp. 797-804 ◽  
Author(s):  
Qinglong Tan ◽  
Maosong Qiu ◽  
Di Cao ◽  
Tianqin Xiong ◽  
Lei Zhang ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Adenosine Diphosphate ◽  
Significant Inhibition ◽  
Triterpene Saponins ◽  
Rabbit Plasma ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity ◽  
Ilex Pubescens ◽  
New Compounds

AbstractTwo new triterpenes and five new triterpene saponins, named ilexpusons A–G (1–7), as well as eight known compounds were isolated from Ilex pubescens. The structures of the new compounds were established by a combination of chemical and spectroscopic methods, including HRESIMS, 1H-NMR, 13C-NMR, 1H-1H COSY, HSQC, HMBC, and NOESY. Additionally, the biological activity of compounds 1 – 15 against adenosine diphosphate-induced platelet aggregation in rabbit plasma was determined. Among the tested compounds, 1, 2, 5, 6, 8, 13, 14, and 15 exhibited significant inhibition of platelet aggregation in vitro.

scholarly journals Inhibitory Effects of Two Ferulates from Angelica Sinensis on Platelet Aggregation and Oxytocin-induced Uterine Contraction

2009 ◽  
Vol 2 (1) ◽  
pp. 43-46 ◽  
Author(s):  
Y. Yu ◽  
B. Q. Lin ◽  
L. Yu ◽  
Y. Q. Hua ◽  
J. A. Duan ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Uterine Contraction ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Biologically Active ◽  
Angelica Sinensis ◽  
Hydrophobic Property ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity

Ferulic acid (FA) is widely considered as a biologically active component in Angelica sinensis, and used as one of the marker compounds for the quality control of Angelica sinensis. However, in A. sinensis, FA mainly exists as its ester, coniferyl ferulate (CF). CF is unstable and readily hydrolyzed into FA during conventional extraction. Herein, their antiplatelet aggregation activities and relaxant effects on oxytocin-induced mouse uterine muscle contraction were investigated and compared. The results showed that FA inhibited arachidonic acid (AA), adenosine diphosphate (ADP) and thrombin (THR)-induced platelet aggregation with IC50 values of 974.8 ± 97.5, 737.9 ± 40.2 and 244.6 ± 25.6 μg/ml, respectively. The potency of CF is much higher than that of FA, and the IC50 values for AA, ADP and THR were 7.1 ± 0.3, 276.4 ± 53.4 and 77.5 ± 23.1 μg/ml, respectively. IC50 of FA was 23.8 ± 6.2 μg/ml for oxytocin-induced uterine contraction in vitro. CF could only be tested at low concentration and its IC50 could not be calculated thereafter because of its strong hydrophobic property. So CF has more potent antiplatelet aggregation activity, while FA has stronger inhibitory effect on oxytocin-induced uterine contraction in vitro

scholarly journals Synthesis of 3,15-Disuccinate-12-Coumarin Substituted Andrographolide Derivatives and Their Antiplatelet Aggregation Activities In Vitro

2020 ◽  
Vol 15 (5) ◽  
pp. 1934578X2091086
Author(s):  
Xue Li ◽  
Jiang-Wei Wang ◽  
Bin Huang ◽  
Zhi-Xiang Peng ◽  
Yuan-Yuan Zhang ◽  
...  
Keyword(s):  
Adenosine Diphosphate ◽  
Biological Evaluation ◽  
Significant Inhibition ◽  
Inhibition Activity ◽  
Antiplatelet Aggregation ◽  
Candidate Structure ◽  
Dependent Behavior ◽  
Aggregation Activity ◽  
Dose Dependent

In order to develop a series of novel compounds with antiplatelet aggregation activities, 3,15-disuccinate-12-coumarin substituted derivatives were designed and synthesized based on the natural product andrographolide. In vitro antiplatelet aggregation activities were evaluated by the turbidimetric method with thrombin, adenosine diphosphate (ADP), arachidonic acid (AA), and collagen as inducers. The biological evaluation revealed that compound 11k showed significant inhibition activity for thrombin, AA, and collagen-induced platelet aggregation at the same time and exhibited a dose-dependent behavior. Compound 11c showed the highest antiplatelet aggregation activity induced by ADP. Most of the derivatives had no significant cytotoxicity. Therefore, our work proved that 3,15-disuccinate-12-coumarin substituted andrographolide derivatives had the potential to become a novel candidate structure for antiplatelet aggregation and deserved further study.

Effects of Lead Acetate on Platelet Aggregation, Ultrastructure and Serotonin Release

1971 ◽  
Vol 26 (03) ◽  
pp. 455-466 ◽  
Author(s):  
R. B Davis ◽  
G. C Holtz
Keyword(s):  
Platelet Aggregation ◽  
Platelet Function ◽  
Lead Acetate ◽  
Platelet Rich Plasma ◽  
Adenosine Diphosphate ◽  
Blood Platelet ◽  
Human Platelets ◽  
Serotonin Release ◽  
Aggregation Of Platelets

SummaryThe effects of lead on blood platelet function and ultrastructure have been investigated. Lead acetate was injected intravenously in 27 rats and was added to rat and human platelet rich plasma in vitro. In vitro studies showed that concentrations of 2.5 × 10-3 M lead acetate reduced or blocked aggregation of rat and human platelets by adenosine diphosphate, collagen, and thrombin. Radioactive serotonin release from human platelets was inhibited by 10-4 M lead acetate. One hour after the injection of lead, platelet aggregation by thrombin was reduced, but platelet aggregation by adenosine diphosphate and collagen showed little change. Three days after lead, aggregation of platelets by collagen and thrombin was blocked and aggregation by adenosine diphosphate reduced. Thrombocytopenia was present 4 days after intravenous lead acetate. Electron micrographs of platelets showed that the mean number of mitochondria per platelet was increased, whereas alpha granules were reduced. Dense bodies were not significantly changed. Lead acetate affects platelet function in concentrations reported in human bone marrow in lead poisoning, and may relate to the binding of free sulfhydryl groups by lead.

scholarly journals Phenolic Chemical Composition of Petroselinum Crispum Extract and Its Effect on Haemostasis

2011 ◽  
Vol 6 (7) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Douglas S. A. Chaves ◽  
Flávia S. Frattani ◽  
Mariane Assafim ◽  
Ana Paula de Almeida ◽  
Russolina B. Zingali ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Chemical Composition ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
The Other ◽  
Petroselinum Crispum ◽  
In Vitro Activity ◽  
Antiplatelet Aggregation ◽  
Aggregation Activity

From the aqueous extract (Pc) of Petroselinum crispum (Mill) flat leaves specimens were isolated and identified the flavonoids apigenin (1), apigenin-7- O-glucoside or cosmosiin (2), apigenin-7- O-apiosyl-(1→2)- O-glucoside or apiin (3) and the coumarin 2″,3″-dihydroxy-furanocoumarin or oxypeucedanin hydrate (4). The inhibitory activity toward clotting formation and platelet aggregation was assessed for Pc flavonoids (1) and (2), and the coumarin (4). Pc showed no inhibition on clotting activity when compared with the control. On the other hand, a strong antiplatelet aggregation activity was observed for Pc (IC50 = 1.81 mg/mL), apigenin (IC50 = 0.036 mg/mL) and cosmosiin (IC50 = 0.18 mg/mL). In all cases ADP was used as inductor of platelet aggregation. Our results showed that Pc, apigenin and cosmosiin interfere on haemostasis inhibiting platelet aggregation. To the best of our knowledge this is the first report for the cosmosiin antiplatelet aggregation in vitro activity.

scholarly journals HEPATOPROTECTIVE ACTIVITY OF VARIOUS EXTRACTS OF CLAUSENA DENTATA (WILLD.) ROEM. (SYN. CLAUSENA WILLDENOVII WIGHT. AND ARN.) RUTACEAE

2017 ◽  
Vol 10 (10) ◽  
pp. 310
Author(s):  
Raju Kamaraj ◽  
Annamalai Maduram ◽  
Raman N
Keyword(s):  
Tamil Nadu ◽  
Stem Bark ◽  
Treated Group ◽  
Hepatoprotective Activity ◽  
Histopathological Changes ◽  
Glutamic Oxaloacetic Transaminase ◽  
Pharmacological Activities ◽  
Treatment Of Wounds ◽  
Trees And Shrubs ◽  
Residual Plant

  Objectives: Clausena (Rutaceae) is a genus of about 23 species of unarmed trees and shrubs. The stem bark of Clausena dentata is used in veterinary medicine for the treatment of wounds and sprains. Even though C. dentata has a lot of potential medical uses, the study on pharmacological activities is in scarce. The present study was undertaken hepatoprotective activity of various extracts of C. dentata. Methods: The plant C. dentata was collected from Kadagaman, near Tiruvannamalai, Tamil Nadu, India. The dry powder of stem bark (2.5 kg) was first soaked in hexane for 24 hrs. The extract was suction filtered. This was repeated for two more days, and similar extracts were pooled together and concentrated at 40°C using Buchi R - 153 Rotavapor. The residual plant material was extracted successively with chloroform and methanol same manner. Preliminary phytochemical test and hepatoprotective activity of various extracts of C. dentata against carbon tetrachloride (CCl4) induced hepatotoxicity in rats were carried out. Biochemical and histopathological changes were observed.Results: The highly significant (p<0.01) reduction in the levels of serums glutamic oxaloacetic transaminase, glutamic pyruvic transaminase, alkaline phosphatase, and bilirubin observed in the study in rats simultaneously treated with C. dentata extracts and CCl4 as compared to CCl4 alone treated.Conclusion: CCl4 induced hepatic damage was counteracted by the extracts of C. dentata. Changes were observed in enzymatic and histopathological level, when compared to CCl4 alone treated group. 

Effect of Dipyridamole on Spontaneous Platelet Aggregation in Whole Blood Decreases with the Time After Venepuncture: Evidence for the Role of ADP

1987 ◽  
Vol 58 (02) ◽  
pp. 744-748 ◽  
Author(s):  
A R Saniabadi ◽  
G D O Lowe ◽  
J C Barbenel ◽  
C D Forbes
Keyword(s):  
Platelet Aggregation ◽  
Correlation Coefficient ◽  
Whole Blood ◽  
Blood Platelet ◽  
Inhibitory Effect ◽  
Time Interval ◽  
Adp Receptor ◽  
Spontaneous Platelet Aggregation

SummarySpontaneous platelet aggregation (SPA) was studied in human whole blood at 3, 5, 10, 20, 30, 40 and 60 minutes after venepuncture. Using a whole blood platelet counter, SPA was quantified by measuring the fall in single platelet count upon rollermixing aliquots of citrated blood at 37° C. The extent of SPA increased with the time after venepuncture, with a correlation coefficient of 0.819. The inhibitory effect of dipyridamole (Dipy) on SPA was studied: (a) 10 μM at each time interval; (b) 0.5-100 μM at 3 and 30 minutes and (c) 15 μM in combination with 100 μM adenosine, 8 μM 2-chloroadenosine (2ClAd, an ADP receptor blocker) and 50 μM aspirin. There was a rapid decrease in the inhibitory effect of Dipy with the time after venepuncture; the correlation coefficient was -0.533. At all the concentrations studied, Dipy was more effective at 3 minutes than at 30 minutes after venepuncture. A combination of Dipy with adenosine, 2ClAd or aspirin was a more effective inhibitor of SPA than either drug alone. However, when 15 μM Dipy and 10 μM Ad were added together, the inhibitory effect of Dipy was not increased significantly, suggesting that Dipy inhibits platelet aggregation independent of Ad. The increase in SPA with the time after venepuncture was abolished when blood was taken directly into the anticoagulant containing 5 μM 2ClAd. It is suggested that ADP released from the red blood cells is responsible for the increased platelet aggregability with the time after venepuncture and makes a serious contribution to the artifacts of in vitro platelet function studies.

The Inhibition of Platelet Aggregation by an Aorta Intima Extract

1974 ◽  
Vol 32 (02/03) ◽  
pp. 417-431 ◽  
Author(s):  
A. du P Heyns ◽  
D. J van den Berg ◽  
G. M Potgieter ◽  
F. P Retief
Keyword(s):  
Platelet Aggregation ◽  
Degradation Products ◽  
Adenosine Diphosphate ◽  
Inhibitory Effect ◽  
Protective Role ◽  
Vascular Trauma ◽  
Wear And Tear ◽  
Sequential Addition ◽  
Aggregation Activity

SummaryThe platelet aggregating activity of extracts of different layers of the arterial wall was compared to that of Achilles tendon. Arterial media and tendon extracts, adjusted to equivalent protein content as an index of concentration, aggregated platelets to the same extent but an arterial intima extract did not aggregate platelets. Platelet aggregation induced by collagen could be inhibited by mixing with intima extract, but only to a maximum of about 80%. Pre-mixing adenosine diphosphate (ADP) with intima extracts diminished the platelet aggregation activity of the ADP. Depending on the relationship between ADP and intima extract concentrations aggregating activity could either be completely inhibited or inhibition abolished. Incubation of ADP with intima extract and subsequent separation of degradation products by paper chromatography, demonstrated a time-dependent breakdown of ADP with AMP, adenosine, inosine and hypoxanthine as metabolic products; ADP removal was complete. Collagen, thrombin and adrenaline aggregate platelets mainly by endogenous ADP of the release reaction. Results of experiments comparing inhibition of aggregation caused by premixing aggregating agent with intima extract, before exposure to platelets, and the sequential addition of first the intima extract and then aggregating agent to platelets, suggest that the inhibitory effect of intima extract results from ADP breakdown. It is suggested that this ADP degradation by intima extract may play a protective role in vivo by limiting the size of platelet aggregates forming at the site of minimal “wear and tear” vascular trauma.

The Effects of Brinolase (Fibrinolytic Enzyme from Aspergillus Oryzae) on Platelet Aggregation of Dog and Man

1972 ◽  
Vol 28 (01) ◽  
pp. 031-048 ◽  
Author(s):  
W. H. E Roschlau ◽  
R Gage
Keyword(s):  
Platelet Aggregation ◽  
Aspergillus Oryzae ◽  
Degradation Products ◽  
Blood Platelet ◽  
Human Platelets ◽  
Fibrinolytic Enzyme ◽  
Inhibitory Effects ◽  
Blood Platelet Aggregation

SummaryInhibition of blood platelet aggregation by brinolase (fibrinolytic enzyme from Aspergillus oryzae) has been demonstrated with human platelets in vitro and with dog platelets in vivo and in vitro, using both ADP and collagen as aggregating stimuli. It is suggested that the optimal inhibitory effects of brinolase occur indirectly through the generation of plasma fibrinogen degradation products, without compromising platelet viability, rather than by direct proteolysis of platelet structures.

Platelet Aggregation Induced in Vitro by Therapeutic Ultrasound

1977 ◽  
Vol 38 (03) ◽  
pp. 0640-0651 ◽  
Author(s):  
B. V Chater ◽  
A. R Williams
Keyword(s):  
Platelet Aggregation ◽  
Direct Action ◽  
Adenosine Diphosphate ◽  
Ultrasonic Cavitation ◽  
Related Phenomenon ◽  
Release Reaction ◽  
Physical Conditions ◽  
Platelet Aggregates ◽  
Active Substances

SummaryPlatelets were found to aggregate spontaneously when exposed to ultrasound generated by a commercial therapeutic device. At a given frequency, aggregation was found to be a dose-related phenomenon, increasing intensities of ultrasound inducing more extensive and more rapid aggregation. At any single intensity, the extent aggregation was increased as the frequency of the applied ultrasound was decreased (from 3.0 to 0.75 MHz).Ultrasound-induced platelet aggregation was found to be related to overall platelet sensitivity to adenosine diphosphate. More sensitive platelets were found to aggregate spontaneously at lower intensities of sound, and also the maximum extent of aggregation was found to be greater. Examination of ultrasound-induced platelet aggregates by electron microscopy demonstrated that the platelets had undergone the release reaction.The observation that haemoglobin was released from erythrocytes in whole blood irradiated under identical physical conditions suggests that the platelets are being distrupted by ultrasonic cavitation (violent gas/bubble oscillation).It is postulated that overall platelet aggregation is the result of two distinct effects. Firstly, the direct action of ultrasonic cavitation disrupts a small proportion of the platelet population, resulting in the liberation of active substances. These substances produce aggregation, both directly and indirectly by inducing the physiological release reaction in adjacent undamaged platelets.

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